The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

Compounds and compositions are provided that can inhibit microsomal prostaglandin E synthase-1 (mPGES-1). The compounds and compositions can reduce inflammation in a subject, such as inflammation caused by an inflammation disorder or symptoms thereof. Pharmaceutical compositions comprising the compound are also provided. Furthermore, methods are provided for reducing inflammation and/or inhibiting mPGES-1. The methods can comprise administering an effective amount of the composition to a subject.

Compounds and compositions are provided that can inhibit microsomal prostaglandin E synthase-1 (mPGES-1). The compounds and compositions can reduce inflammation in a subject, such as inflammation caused by an inflammation disorder or symptoms thereof. Pharmaceutical compositions comprising the compound are also provided. Furthermore, methods are provided for reducing inflammation and/or inhibiting mPGES-1. The methods can comprise administering an effective amount of the composition to a subject.

An object is to provide a novel bismaleimide compound. The solution is a bismaleimide compound represented by formula (1):

##STR00001## wherein A.sub.1 represents a direct bond, a divalent linking group represented by formula (1-1), (1-2), or (1-3):

##STR00002## wherein ring a represents a benzene ring or a cyclohexane ring; X represents a direct bond or a divalent linking group; and Z represents a monovalent substituent; or a divalent linking group other than this; at least one of a plurality of A.sub.1s is formula (1-1), (1-2), or (1-3); A.sub.2 represents a divalent linking group that is a residue of a saturated aliphatic dicarboxylic acid compound, a divalent linking group that is a residue of an aromatic dicarboxylic acid compound, or a divalent linking group other than this; and when A.sub.2 is present singly, A.sub.2 is a divalent linking group that is a residue of a saturated aliphatic dicarboxylic acid compound, and when a plurality of A.sub.2s is present, at least one of A.sub.2s is a divalent linking group that is a residue of a saturated aliphatic dicarboxylic acid compound.

An object is to provide a novel bismaleimide compound. The solution is a bismaleimide compound represented by formula (1):

##STR00001## wherein A.sub.1 represents a direct bond, a divalent linking group represented by formula (1-1), (1-2), or (1-3):

##STR00002## wherein ring a represents a benzene ring or a cyclohexane ring; X represents a direct bond or a divalent linking group; and Z represents a monovalent substituent; or a divalent linking group other than this; at least one of a plurality of A.sub.1s is formula (1-1), (1-2), or (1-3); A.sub.2 represents a divalent linking group that is a residue of a saturated aliphatic dicarboxylic acid compound, a divalent linking group that is a residue of an aromatic dicarboxylic acid compound, or a divalent linking group other than this; and when A.sub.2 is present singly, A.sub.2 is a divalent linking group that is a residue of a saturated aliphatic dicarboxylic acid compound, and when a plurality of A.sub.2s is present, at least one of A.sub.2s is a divalent linking group that is a residue of a saturated aliphatic dicarboxylic acid compound.

A PEG linker as represented by formula (I), wherein n and m are respectively an integer from 1 to 7, providing the PEG linker with 1 to 49 linking sites. A ligand drug conjugate as represented by formula (II). The conjugate uses the PEG linker to increase a drug loading capacity and drug loading diversity, thereby improving pharmaceutical efficacy.
Y1-PEG1-{R.sup.1-PEG2-{Y4}.sub.n}.sub.m  (I)
TM-{R.sup.2-PEG1-{R.sup.1-PEG2-{R.sup.3-A′-drug}.sub.n}.sub.m}.sub.l  (II)

A PEG linker as represented by formula (I), wherein n and m are respectively an integer from 1 to 7, providing the PEG linker with 1 to 49 linking sites. A ligand drug conjugate as represented by formula (II). The conjugate uses the PEG linker to increase a drug loading capacity and drug loading diversity, thereby improving pharmaceutical efficacy.
Y1-PEG1-{R.sup.1-PEG2-{Y4}.sub.n}.sub.m  (I)
TM-{R.sup.2-PEG1-{R.sup.1-PEG2-{R.sup.3-A′-drug}.sub.n}.sub.m}.sub.l  (II)

The present invention provides a film forming material for lithography comprising a compound having: a group of formula (0A):

##STR00001## and a group of formula (0B):

##STR00002##

wherein each R is independently selected from the group consisting of a hydrogen atom and an alkyl group having 1 to 4 carbon atoms, provided that at least one R is an alkyl group having 1 to 4 carbon atoms.

The present invention provides a film forming material for lithography comprising a compound having: a group of formula (0A):

##STR00001## and a group of formula (0B):

##STR00002##

wherein each R is independently selected from the group consisting of a hydrogen atom and an alkyl group having 1 to 4 carbon atoms, provided that at least one R is an alkyl group having 1 to 4 carbon atoms.

Provided herein are novel ortho-Phthalaldehyde (OPA) containing linkers (OPA-L) and the use of OPA-L for the preparation of Antibody-drug conjugate (ADC) via the formation of Phthalimidine through the reaction of primary amine on antibody (e.g., residue of Lysine) and ortho-Phthalaldehyde. The advantage of this OPA-L is high reactivity and can be applied in different types of antibodies to form stably-linked conjugates. The use of OPA-L for the preparation of ADC is advantageous for mild and wide condition of conjugation, for instance, low percentage of organic solvent required, wide range of pH and temperature can be used.